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1. 发明授权

US09242937B2 Pharmaceutically active disubstituted pyridine derivatives 有权
标题翻译：药用活性二取代吡啶衍生物
公开(公告)号：US09242937B2
公开(公告)日：2016-01-26
申请号：US14002731
申请日：2012-03-01
申请人： Gerd Rühter , Peter Nussbaumer , Axel Choidas , Carsten Schulz-Fademrecht , Bert Klebl , Jan Eickhoff
发明人： Gerd Rühter , Peter Nussbaumer , Axel Choidas , Carsten Schulz-Fademrecht , Bert Klebl , Jan Eickhoff
IPC分类号： C07D211/72 , C07D213/74 , A61K31/4418 , A61K45/06
CPC分类号： C07D213/74 , A61K31/4418 , A61K45/06
摘要： The present invention relates to disubstituted pyridine derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of infectious diseases, including opportunistic diseases, immunological diseases, autoimmune diseases, cardiovascular diseases, cell proliferative diseases, inflammation, erectile dysfunction and stroke, and pharmaceutical compositions containing at least one of said disubstituted pyridine derivatives and/or pharmaceutically acceptable salts thereof. Furthermore, the present invention relates to the use of said disubstituted pyridine derivatives as inhibitors for a protein kinase.
摘要翻译：本发明涉及二取代的吡啶衍生物和/或其药学上可接受的盐，这些衍生物作为药物活性剂的用途，特别是用于预防和/或治疗感染性疾病，包括机会性疾病，免疫疾病，自身免疫性疾病，心血管疾病，细胞增殖性疾病，炎症，勃起功能障碍和中风，以及含有至少一种所述二取代吡啶衍生物和/或其药学上可接受的盐的药物组合物。此外，本发明涉及所述二取代的吡啶衍生物作为蛋白激酶的抑制剂的用途。

2. 发明申请

US20140296304A1 Pharmaceutically Active Disubstituted Pyridine Derivatives 有权
标题翻译：药学活性二取代吡啶衍生物
公开(公告)号：US20140296304A1
公开(公告)日：2014-10-02
申请号：US14002731
申请日：2012-03-01
申请人： Gerd Rühter , Peter Nussbaumer , Axel Choidas , Carsten Schulz-Fademrecht , Bert Klebl , Jan Eickhoff
发明人： Gerd Rühter , Peter Nussbaumer , Axel Choidas , Carsten Schulz-Fademrecht , Bert Klebl , Jan Eickhoff
IPC分类号： C07D213/74 , A61K45/06 , A61K31/4418
CPC分类号： C07D213/74 , A61K31/4418 , A61K45/06
摘要： The present invention relates to disubstituted pyridine derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of infectious diseases, including opportunistic diseases, immunological diseases, autoimmune diseases, cardiovascular diseases, cell proliferative diseases, inflammation, erectile dysfunction and stroke, and pharmaceutical compositions containing at least one of said disubstituted pyridine derivatives and/or pharmaceutically acceptable salts thereof. Furthermore, the present invention relates to the use of said disubstituted pyridine derivatives as inhibitors for a protein kinase.
摘要翻译：本发明涉及二取代的吡啶衍生物和/或其药学上可接受的盐，这些衍生物作为药物活性剂的用途，特别是用于预防和/或治疗感染性疾病，包括机会性疾病，免疫疾病，自身免疫性疾病，心血管疾病，细胞增殖性疾病，炎症，勃起功能障碍和中风，以及含有至少一种所述二取代吡啶衍生物和/或其药学上可接受的盐的药物组合物。此外，本发明涉及所述二取代的吡啶衍生物作为蛋白激酶的抑制剂的用途。

3. 发明授权

US09226929B2 Pharmaceutically active disubstituted triazine derivatives 有权
标题翻译：药用活性二取代三嗪衍生物
公开(公告)号：US09226929B2
公开(公告)日：2016-01-05
申请号：US14002730
申请日：2012-03-01
申请人： Gerd Rühter , Uwe Koch , Peter Nussbaumer , Carsten Schulz-Fademrecht , Jan Eickhoff
发明人： Gerd Rühter , Uwe Koch , Peter Nussbaumer , Carsten Schulz-Fademrecht , Jan Eickhoff
IPC分类号： C07D251/12 , C07D401/04 , C07D403/04 , C07D513/04 , A61K31/5377 , A61K31/53 , A61K31/5355 , C07D251/48 , C07D471/04 , C07D487/04 , C07D495/04 , A61K45/06 , C07D403/14 , C07D413/04
CPC分类号： A61K31/5377 , A61K31/53 , A61K31/5355 , A61K45/06 , C07D251/48 , C07D401/04 , C07D403/04 , C07D403/14 , C07D413/04 , C07D471/04 , C07D487/04 , C07D495/04 , C07D513/04 , A61K2300/00
摘要： The present invention relates to disubstituted triazine derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of infectious diseases, including opportunistic diseases, immunological diseases, autoimmune diseases, cardiovascular diseases, cell proliferative diseases, inflammation, erectile dysfunction and stroke, and pharmaceutical compositions containing at least one of said disubstituted triazine derivatives and/or pharmaceutically acceptable salts thereof. Furthermore, the present invention relates to the use of said disubstituted triazine derivatives as inhibitors for a protein kinase.
摘要翻译：本发明涉及二取代的三嗪衍生物和/或其药学上可接受的盐，这些衍生物作为药物活性剂的用途，特别是用于预防和/或治疗感染性疾病，包括机会性疾病，免疫疾病，自身免疫性疾病，心血管疾病，细胞增殖性疾病，炎症，勃起功能障碍和中风，以及含有至少一种所述二取代的三嗪衍生物和/或其药学上可接受的盐的药物组合物。此外，本发明涉及所述二取代三嗪衍生物作为蛋白激酶的抑制剂的用途。

4. 发明申请

US20140179662A1 PHARMACEUTICALLY ACTIVE DISUBSTITUTED TRIAZINE DERIVATIVES 有权
标题翻译：药物动力学分析的TRIAZINE衍生物
公开(公告)号：US20140179662A1
公开(公告)日：2014-06-26
申请号：US14002730
申请日：2012-03-01
申请人： Gerd Rühter , Uwe Koch , Peter Nussbaumer , Carsten Schulz-Fademrecht , Jan Eickhoff
发明人： Gerd Rühter , Uwe Koch , Peter Nussbaumer , Carsten Schulz-Fademrecht , Jan Eickhoff
IPC分类号： C07D513/04 , C07D401/04 , A61K31/53 , C07D413/04 , C07D487/04 , C07D403/04 , C07D403/14 , C07D471/04 , C07D495/04 , A61K45/06 , A61K31/5377
CPC分类号： A61K31/5377 , A61K31/53 , A61K31/5355 , A61K45/06 , C07D251/48 , C07D401/04 , C07D403/04 , C07D403/14 , C07D413/04 , C07D471/04 , C07D487/04 , C07D495/04 , C07D513/04 , A61K2300/00
摘要： The present invention relates to disubstituted triazine derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of infectious diseases, including opportunistic diseases, immunological diseases, autoimmune diseases, cardiovascular diseases, cell proliferative diseases, inflammation, erectile dysfunction and stroke, and pharmaceutical compositions containing at least one of said disubstituted triazine derivatives and/or pharmaceutically acceptable salts thereof. Furthermore, the present invention relates to the use of said disubstituted triazine derivatives as inhibitors for a protein kinase.
摘要翻译：本发明涉及二取代的三嗪衍生物和/或其药学上可接受的盐，这些衍生物作为药物活性剂的用途，特别是用于预防和/或治疗感染性疾病，包括机会性疾病，免疫疾病，自身免疫性疾病，心血管疾病，细胞增殖性疾病，炎症，勃起功能障碍和中风，以及含有至少一种所述二取代的三嗪衍生物和/或其药学上可接受的盐的药物组合物。此外，本发明涉及所述二取代三嗪衍生物作为蛋白激酶的抑制剂的用途。

5. 发明申请

US20130079345A1 PHARMACEUTICALLY ACTIVE DISUBSTITUTED TRIAZINE DERIVATIVES 审中-公开
标题翻译：药物动力学分析的TRIAZINE衍生物
公开(公告)号：US20130079345A1
公开(公告)日：2013-03-28
申请号：US13636448
申请日：2011-03-20
申请人： Jan Eickhoff , Peter Nussbaumer , Gerd Ruhter , Carsten Schultz-Fademrecht , Ulrich Lucking , Axel Choidas , Bert Klebl
发明人： Jan Eickhoff , Peter Nussbaumer , Gerd Ruhter , Carsten Schultz-Fademrecht , Ulrich Lucking , Axel Choidas , Bert Klebl
IPC分类号： C07D251/16 , C07D405/10 , C07D401/12 , A61K45/06 , C07D413/10 , A61K31/5377 , C07D401/10 , C07D403/12 , A61K31/53 , C07D401/04
CPC分类号： C07D251/16 , A61K31/53 , A61K31/5377 , A61K45/06 , C07D251/22 , C07D401/04 , C07D401/10 , C07D401/12 , C07D403/12 , C07D405/10 , C07D407/04 , C07D413/10
摘要： The present invention relates to disubstituted triazine derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of infectious diseases, including opportunistic diseases, immunological diseases, autoimmune diseases, cardiovascular diseases, cell proliferative diseases, inflammation, erectile dysfunction and stroke, and pharmaceutical compositions containing at least one of said disubstituted triazine derivatives and/or pharmaceutically acceptable salts thereof. Furthermore, the present invention relates to the use of said disubstituted triazine derivatives as inhibitors for a protein kinase.
摘要翻译：本发明涉及二取代的三嗪衍生物和/或其药学上可接受的盐，这些衍生物作为药物活性剂的用途，特别是用于预防和/或治疗感染性疾病，包括机会性疾病，免疫疾病，自身免疫性疾病，心血管疾病，细胞增殖性疾病，炎症，勃起功能障碍和中风，以及含有至少一种所述二取代的三嗪衍生物和/或其药学上可接受的盐的药物组合物。此外，本发明涉及所述二取代三嗪衍生物作为蛋白激酶的抑制剂的用途。

6. 发明授权

US08999982B2 Pharmaceutically active compounds as Axl inhibitors 有权
标题翻译：作为Axl抑制剂的药物活性化合物
公开(公告)号：US08999982B2
公开(公告)日：2015-04-07
申请号：US13819560
申请日：2011-08-26
申请人： Carsten Schultz-Fademrecht , Bert Klebl , Axel Choidas , Uwe Koch , Jan Eickhoff , Alexander Wolf , Axel Ullrich
发明人： Carsten Schultz-Fademrecht , Bert Klebl , Axel Choidas , Uwe Koch , Jan Eickhoff , Alexander Wolf , Axel Ullrich
IPC分类号： A61K31/495 , A61K31/47 , C07D401/12 , C07D401/14 , C07D417/12 , C07D417/14 , C07D413/12 , C07D413/14 , C07D215/233
CPC分类号： C07D401/12 , A61K31/47 , A61K31/495 , C07D215/233 , C07D401/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： The present invention relates to 1-nitrogen-heterocyclic-2-carboxamides and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the treatment and/or prevention of Axl receptor tyrosine kinase subfamily induced disorders, including cancer and primary tumor metastases, and pharmaceutical compositions containing at least one of said 1-nitrogen-heterocyclic-2-carboxamide derivatives and/or pharmaceutically acceptable salts thereof.
摘要翻译：本发明涉及1-氮杂环-2-甲酰胺和/或其药学上可接受的盐，这些衍生物用作药物活性剂，特别是用于治疗和/或预防Axl受体酪氨酸激酶亚家族诱导的病症，包括癌症和原发性肿瘤转移，以及含有至少一种所述1-氮杂环-2-甲酰胺衍生物和/或其药学上可接受的盐的药物组合物。

7. 发明申请

US20140018365A1 PHARMACEUTICALLY ACTIVE COMPOUNDS AS AXL INHIBITORS 有权
标题翻译：药物活性化合物作为AXL抑制剂
公开(公告)号：US20140018365A1
公开(公告)日：2014-01-16
申请号：US13819560
申请日：2011-08-26
申请人： Carsten Schultz-Fademrecht , Bert Klebl , Axel Choidas , Uwe Koch , Jan Eickhoff , Alexander Wolf , Axel Ullrich
发明人： Carsten Schultz-Fademrecht , Bert Klebl , Axel Choidas , Uwe Koch , Jan Eickhoff , Alexander Wolf , Axel Ullrich
IPC分类号： C07D401/12 , C07D215/233 , C07D417/12 , C07D413/14 , C07D417/14 , C07D401/14
CPC分类号： C07D401/12 , A61K31/47 , A61K31/495 , C07D215/233 , C07D401/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： The present invention relates to 1-nitrogen-heterocyclic-2-carboxamides and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the treatment and/or prevention of Axl receptor tyrosine kinase subfamily induced disorders, including cancer and primary tumor metastases, and pharmaceutical compositions containing at least one of said 1-nitrogen-heterocyclic-2-carboxamide derivatives and/or pharmaceutically acceptable salts thereof.
摘要翻译：本发明涉及1-氮杂环-2-甲酰胺和/或其药学上可接受的盐，这些衍生物用作药物活性剂，特别是用于治疗和/或预防Axl受体酪氨酸激酶亚家族诱导的病症，包括癌症和原发性肿瘤转移，以及含有至少一种所述1-氮杂环-2-甲酰胺衍生物和/或其药学上可接受的盐的药物组合物。

8. 发明申请

US20140287454A1 SUSCEPTIBILITY TO SELECTIVE CDK9 INHIBITORS 审中-公开
标题翻译：选择性CDK9抑制剂的缺点
公开(公告)号：US20140287454A1
公开(公告)日：2014-09-25
申请号：US14240315
申请日：2012-08-22
申请人： Axel Choidas , Bert Klebl , Peter Habenberger , Jan Eickhoff , Roman Thomas , Johannes Heuckmann
发明人： Axel Choidas , Bert Klebl , Peter Habenberger , Jan Eickhoff , Roman Thomas , Johannes Heuckmann
IPC分类号： G01N33/50
CPC分类号： G01N33/5011 , C12Q1/6881 , C12Q1/6886 , C12Q2600/106 , G01N2800/52
摘要： The present invention relates to a method of selecting (a) cell(s), (a) tissue(s) or (a) cell culture(s) with susceptibility to a selective CDK9 inhibitor. Also a method for determining the responsiveness of a mammalian tumor cell or cancer cell to treatment with a selective CDK9 inhibitor is described herein. In particular, the present invention provides for an in vitro method for the identification of a responder for or a patient sensitive to a selective CDK9 inhibitor, whereby the patient is suspected to suffer from NUT midline carcinoma (NMC). The present invention also relates to a method of monitoring or predicting the efficacy of a treatment of NUT midline carcinoma (NMC), wherein treatment with a selective CDK9 inhibitor is in particular envisaged. Also the use of a (transgenic) non-human animal or a (transgenic) cell having at least one rearrangement in the NUT gene for screening and/or validation of a medicament for the treatment NUT midline carcinoma (NMC) is described. Furthermore, a kit useful for carrying out the methods described herein as well as an oligo- or polynucleotide capable of detecting rearrangements in the NUT gene are provided.
摘要翻译：本发明涉及一种选择（a）对选择性CDK9抑制剂具有易感性的细胞，（a）组织或（a）细胞培养物的方法。本文还描述了确定哺乳动物肿瘤细胞或癌细胞对用选择性CDK9抑制剂进行治疗的反应性的方法。特别地，本发明提供了用于鉴定对选择性CDK9抑制剂敏感的患者或患者的体外方法，由此患者怀疑患有NUT中线癌（NMC）。本发明还涉及监测或预测NUT中线癌（NMC）治疗功效的方法，其中特别设想用选择性CDK9抑制剂进行治疗。还描述了在NUT基因中具有至少一个重排的（转基因）非人动物或（转基因）细胞用于筛选和/或验证用于治疗NUT中线癌（NMC）的药物的用途。此外，提供了可用于实施本文所述方法的试剂盒以及能够检测NUT基因重排的寡核苷酸或多核苷酸。

9. 发明申请

US20150329537A2 CDK9 INHIBITORS IN THE TREATMENT OF MIDLINE CARCINOMA 审中-公开
标题翻译： CDK9抑制剂治疗中性粒细胞减少症
公开(公告)号：US20150329537A2
公开(公告)日：2015-11-19
申请号：US14240329
申请日：2012-08-22
申请人： Axel Choidas , Bert Klebl , Peter Habenberger , Jan Eickhoff , Roman Thomas , Johannes Heuckmann
发明人： Axel Choidas , Bert Klebl , Peter Habenberger , Jan Eickhoff , Roman Thomas , Johannes Heuckmann
IPC分类号： C07D471/04 , C07D405/10 , C07D401/12 , C07D403/04 , C07D403/12 , C07C53/18 , C07D213/40 , C07D251/16 , C07D401/04
CPC分类号： C07C53/18 , A61K31/4418 , A61K31/53 , C07D213/40 , C07D213/74 , C07D251/16 , C07D251/22 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/10 , C07D471/04
摘要： The present invention relates to a CDK9 inhibitor, especially a selective CDK9 inhibitor, for use in treating, ameliorating and/or preventing midline carcinoma. Also corresponding methods for treating, preventing or ameliorating midline carcinoma are subject of the present invention. Preferably, NUT midline carcinoma is treated with the CDK9 inhibitors in accordance with the present invention.
摘要翻译：本发明涉及用于治疗，改善和/或预防中线癌症的CDK9抑制剂，特别是选择性CDK9抑制剂。用于治疗，预防或改善中线癌的相应方法也是本发明的主题。优选地，根据本发明，用CDK9抑制剂处理NUT中线癌。

10. 发明申请

US20140303167A1 CDK9 INHIBITORS IN THE TREATMENT OF MIDLINE CARCINOMA 审中-公开
标题翻译： CDK9抑制剂治疗中性粒细胞减少症
公开(公告)号：US20140303167A1
公开(公告)日：2014-10-09
申请号：US14240329
申请日：2012-08-22
申请人： Axel Choidas , Bert Klebl , Peter Habenberger , Jan Eickhoff , Roman Thomas , Johannes Heuckmann
发明人： Axel Choidas , Bert Klebl , Peter Habenberger , Jan Eickhoff , Roman Thomas , Johannes Heuckmann
IPC分类号： C07D471/04 , C07D405/10 , C07D401/12 , C07D403/04 , C07D403/12 , C07C53/18 , C07D213/40 , C07D251/16 , C07D401/04
CPC分类号： C07C53/18 , A61K31/4418 , A61K31/53 , C07D213/40 , C07D213/74 , C07D251/16 , C07D251/22 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/10 , C07D471/04
摘要： The present invention relates to a CDK9 inhibitor, especially a selective CDK9 inhibitor, for use in treating, ameliorating and/or preventing midline carcinoma. Also corresponding methods for treating, preventing or ameliorating midline carcinoma are subject of the present invention. Preferably, NUT midline carcinoma is treated with the CDK9 inhibitors in accordance with the present invention.
摘要翻译：本发明涉及用于治疗，改善和/或预防中线癌症的CDK9抑制剂，特别是选择性CDK9抑制剂。用于治疗，预防或改善中线癌的相应方法也是本发明的主题。优选地，根据本发明，用CDK9抑制剂处理NUT中线癌。

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